CN112218867B - 腺苷受体拮抗剂及其用途 - Google Patents

腺苷受体拮抗剂及其用途 Download PDF

Info

Publication number
CN112218867B
CN112218867B CN201980030563.6A CN201980030563A CN112218867B CN 112218867 B CN112218867 B CN 112218867B CN 201980030563 A CN201980030563 A CN 201980030563A CN 112218867 B CN112218867 B CN 112218867B
Authority
CN
China
Prior art keywords
substituted
unsubstituted
compound
alkyl
group
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
CN201980030563.6A
Other languages
English (en)
Chinese (zh)
Other versions
CN112218867A (zh
Inventor
刘继文
埃尔法蒂赫·埃尔扎因
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Taiang Treatment Co
Original Assignee
Taiang Treatment Co
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Taiang Treatment Co filed Critical Taiang Treatment Co
Publication of CN112218867A publication Critical patent/CN112218867A/zh
Application granted granted Critical
Publication of CN112218867B publication Critical patent/CN112218867B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/04—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
    • C07D473/06—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/08—Solutions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4816—Wall or shell material
    • A61K9/4825—Proteins, e.g. gelatin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • C07F9/65616—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings containing the ring system having three or more than three double bonds between ring members or between ring members and non-ring members, e.g. purine or analogs

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Pulmonology (AREA)
  • Neurosurgery (AREA)
  • Child & Adolescent Psychology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Saccharide Compounds (AREA)
CN201980030563.6A 2018-03-05 2019-03-05 腺苷受体拮抗剂及其用途 Active CN112218867B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201862638737P 2018-03-05 2018-03-05
US62/638,737 2018-03-05
US201862688088P 2018-06-21 2018-06-21
US62/688,088 2018-06-21
PCT/US2019/020810 WO2019173380A1 (en) 2018-03-05 2019-03-05 Adenosine receptor antagonists and uses thereof

Publications (2)

Publication Number Publication Date
CN112218867A CN112218867A (zh) 2021-01-12
CN112218867B true CN112218867B (zh) 2023-11-21

Family

ID=67847428

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201980030563.6A Active CN112218867B (zh) 2018-03-05 2019-03-05 腺苷受体拮抗剂及其用途

Country Status (12)

Country Link
US (3) US20210040097A1 (https=)
EP (2) EP3762386B1 (https=)
JP (2) JP7849948B2 (https=)
KR (1) KR102754522B1 (https=)
CN (1) CN112218867B (https=)
AU (2) AU2019232736B2 (https=)
BR (1) BR112020018158A2 (https=)
ES (1) ES2975753T3 (https=)
IL (1) IL277144B2 (https=)
MX (1) MX2020009286A (https=)
SG (1) SG11202008611UA (https=)
WO (1) WO2019173380A1 (https=)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2975753T3 (es) 2018-03-05 2024-07-12 Teon Therapeutics Inc Antagonistas del receptor de adenosina y usos de los mismos
WO2022032091A1 (en) * 2020-08-07 2022-02-10 Teon Therapeutics, Inc. Combination therapy with adenosine receptor antagonists
CN116322698A (zh) * 2020-09-04 2023-06-23 泰昂治疗公司 腺苷a2b受体拮抗剂的共晶
WO2022256550A1 (en) 2021-06-04 2022-12-08 Teon Therapeutics, Inc. Crystalline forms of an adenosine a2b receptor antagonist
TW202327612A (zh) * 2021-09-10 2023-07-16 美商天恩治療有限公司 使用腺苷受體拮抗劑之改良療法
EP4554943A1 (en) * 2022-07-14 2025-05-21 Teon Therapeutics, Inc. Adenosine receptor antagonists and uses thereof
WO2026035860A1 (en) 2024-08-07 2026-02-12 Teon Therapeutics, Inc. Formulations of adenosine receptor antagonist

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1771250A (zh) * 2003-05-06 2006-05-10 Cv医药有限公司 作为a2b腺苷受体拮抗剂的黄嘌呤衍生物
CN101043889A (zh) * 2004-09-01 2007-09-26 Cv医药有限公司 使用a2b腺苷受体拮抗剂促使伤口愈合的方法
CN101198608A (zh) * 2005-06-16 2008-06-11 Cv医药有限公司 A2b腺苷受体拮抗剂的前药
CN101405003A (zh) * 2006-03-17 2009-04-08 Cv医药有限公司 利用a2b腺苷受体拮抗剂预防和治疗肝病的方法
CN102015712A (zh) * 2008-03-26 2011-04-13 阿德维纳斯治疗私人有限公司 作为腺苷受体拮抗剂的杂环化合物
CN103237548A (zh) * 2010-06-30 2013-08-07 吉利德科学股份有限公司 A2b腺苷受体拮抗剂用于治疗肺高血压的应用
CN103261200A (zh) * 2010-09-13 2013-08-21 阿迪维纳斯疗法有限公司 作为a2b腺苷受体拮抗剂的前药的嘌呤化合物、它们的制备方法及医药用途
CN103582481A (zh) * 2011-04-07 2014-02-12 吉利德科学股份有限公司 A2b腺苷受体拮抗剂用于治疗心肌梗塞后患者的心力衰竭及心律不齐的用途

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5466811A (en) * 1994-07-18 1995-11-14 Merck & Co., Inc. Dioxolenylmethyl carbamates pro moieties for amine drugs
CA2323047C (en) * 1998-04-15 2005-03-15 Warner-Lambert Company Prodrugs of benzofuranylmethyl carbamate nk, antagonists
US20080318983A1 (en) 2001-11-09 2008-12-25 Rao Kalla A2b adenosine receptor antagonists
US6977300B2 (en) 2001-11-09 2005-12-20 Cv Therapeutics, Inc. A2B adenosine receptor antagonists
US7317017B2 (en) 2002-11-08 2008-01-08 Cv Therapeutics, Inc. A2B adenosine receptor antagonists
US7125993B2 (en) 2001-11-09 2006-10-24 Cv Therapeutics, Inc. A2B adenosine receptor antagonists
US7304070B2 (en) 2001-11-09 2007-12-04 Cv Therapeutics, Inc. A2B adenosine receptor antagonists
DK1444233T3 (da) * 2001-11-09 2011-10-17 Gilead Palo Alto Inc A2B-adenosinreceptorantagonister
HRP20040853A2 (en) * 2002-03-20 2004-12-31 Bristol Myers Squibb Co Phosphate prodrugs of fluorooxindoles
EP1799221A1 (en) 2004-10-15 2007-06-27 Cv Therapeutics, Inc. Method of preventing and treating airway remodeling and pulmonary inflammation using a2b adenosine receptor antagonists
WO2008066627A2 (en) 2006-10-24 2008-06-05 Board Of Regents, The University Of Texas System Adenosine signaling in diagnosis, treatment and prevention of priapism and erectile dysfunction
WO2009088518A1 (en) 2008-01-11 2009-07-16 Cv Therapeutics, Inc. A2b adenosine receptor antagonists for the treatment of cancer
WO2009157938A1 (en) 2008-06-26 2009-12-30 Cv Therapeutics, Inc. A2b adenosine receptor antagonists for treating cancer
AU2011270701B2 (en) * 2010-06-24 2015-05-14 Alkermes Pharma Ireland Limited Prodrugs of NH-acidic compounds: ester, carbonate, carbamate and phosphonate derivatives
WO2012170209A2 (en) * 2011-05-23 2012-12-13 Nectid, Inc. Benzofuran-2 carboxamide compounds
US10117868B2 (en) 2011-10-25 2018-11-06 Case Western Reserve University Systems pharmacology for treating ocular disorders
CN111093669A (zh) 2017-08-14 2020-05-01 法斯瑞斯公司 用于治疗癌症的腺苷受体拮抗剂的微颗粒制剂
CN111741752A (zh) 2017-12-19 2020-10-02 Gpcr治疗公司 Gpcr异聚体抑制剂及其用途
ES2975753T3 (es) 2018-03-05 2024-07-12 Teon Therapeutics Inc Antagonistas del receptor de adenosina y usos de los mismos

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1771250A (zh) * 2003-05-06 2006-05-10 Cv医药有限公司 作为a2b腺苷受体拮抗剂的黄嘌呤衍生物
CN101043889A (zh) * 2004-09-01 2007-09-26 Cv医药有限公司 使用a2b腺苷受体拮抗剂促使伤口愈合的方法
CN101198608A (zh) * 2005-06-16 2008-06-11 Cv医药有限公司 A2b腺苷受体拮抗剂的前药
CN101405003A (zh) * 2006-03-17 2009-04-08 Cv医药有限公司 利用a2b腺苷受体拮抗剂预防和治疗肝病的方法
CN102015712A (zh) * 2008-03-26 2011-04-13 阿德维纳斯治疗私人有限公司 作为腺苷受体拮抗剂的杂环化合物
CN103237548A (zh) * 2010-06-30 2013-08-07 吉利德科学股份有限公司 A2b腺苷受体拮抗剂用于治疗肺高血压的应用
CN103261200A (zh) * 2010-09-13 2013-08-21 阿迪维纳斯疗法有限公司 作为a2b腺苷受体拮抗剂的前药的嘌呤化合物、它们的制备方法及医药用途
CN103582481A (zh) * 2011-04-07 2014-02-12 吉利德科学股份有限公司 A2b腺苷受体拮抗剂用于治疗心肌梗塞后患者的心力衰竭及心律不齐的用途

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
STN检索报告1;来源于GVK BIO等;《数据库REGISTRY（在线）》;20111202;CAS登记号：1347593-72-9等 *

Also Published As

Publication number Publication date
AU2019232736B2 (en) 2024-05-02
ES2975753T3 (es) 2024-07-12
KR102754522B1 (ko) 2025-01-13
US20210163483A1 (en) 2021-06-03
US20210040097A1 (en) 2021-02-11
AU2019232736A1 (en) 2020-10-08
IL277144B1 (en) 2024-02-01
JP7849948B2 (ja) 2026-04-22
JP2024032976A (ja) 2024-03-12
WO2019173380A1 (en) 2019-09-12
EP4364727A3 (en) 2024-05-15
AU2024204483B2 (en) 2026-04-02
EP3762386A1 (en) 2021-01-13
KR20200132901A (ko) 2020-11-25
IL277144B2 (en) 2024-06-01
US11124515B2 (en) 2021-09-21
EP3762386A4 (en) 2021-11-24
SG11202008611UA (en) 2020-10-29
CA3093234A1 (en) 2019-09-12
BR112020018158A2 (pt) 2021-02-02
JP2021517164A (ja) 2021-07-15
MX2020009286A (es) 2020-12-11
IL277144A (en) 2020-10-29
CN112218867A (zh) 2021-01-12
EP4364727A2 (en) 2024-05-08
AU2024204483A1 (en) 2024-07-18
US20220056033A1 (en) 2022-02-24
EP3762386B1 (en) 2024-01-24

Similar Documents

Publication Publication Date Title
CN112218867B (zh) 腺苷受体拮抗剂及其用途
JP2022519331A (ja) 複素環化合物およびその用途
JP7429224B2 (ja) Ｌｐａアンタゴニストとしてのシクロヘプチル酸
PL174610B1 (pl) Nowe związki heterocykliczne
BR112020011953A2 (pt) ácidos carbamoil ciclo-hexílicos n-ligados a pirazol como antagonistas de lpa
WO1991009029A1 (en) Therapeutically active chloro substituted benzimidazoles, processes for their preparation as well as their use
KR102791742B1 (ko) (s)-3-아미노-4-(디플루오로메틸레닐)사이클로펜트-1-엔-1-카르복실산의 합성을 위한 공정
EP3428159B1 (en) Crystalline forms of mesylate salt of pyridinyl amino pyrimidine derivative, preparation methods therefor, and applications thereof
US20190135787A1 (en) Pyrimidine compositions, ultra-pure compositions and salts thereof, methods of making the same, and methods of using the same for treating histamine h4 receptor (h4) mediated diseases and conditions
US4619938A (en) Fatty acid derivatives of aminoalkyl nicotinic acid esters and platelet aggregation inhibitors
EP0314275A2 (en) 2-Pyrrolidone-5-carboxylic acid compounds
WO2025236860A1 (zh) 蟾蜍色胺衍生物及其在镇痛、抗抑郁药物中的应用
JP2582406B2 (ja) 新規なキノキサリン誘導体及びそれを含有する坑潰瘍剤
JP2026074199A (ja) アデノシン受容体アンタゴニストおよびその使用
HK40108164A (en) Adenosine receptor antagonists and uses thereof
EA043897B1 (ru) Антагонисты аденозиновых рецепторов и их применения
TWI845843B (zh) 新型吡嗪化合物
HK40041747A (en) Adenosine receptor antagonists and uses thereof
HK40041747B (en) Adenosine receptor antagonists and uses thereof
IE904248A1 (en) Therapeutically active fluoro substituted benzimidazoles,¹processes for their preparation as well as their use
CA3093234C (en) Adenosine receptor antagonists and uses thereof
KR20000075717A (ko) 퀴녹살린디온
JPH01261386A (ja) 新規な２―ピリジルメチルチオ誘導体及びそれを含有する抗潰瘍剤
JPS642596B2 (https=)
JPH0434541B2 (https=)

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
GR01 Patent grant
GR01 Patent grant